Fullerene gallium phosphonate and methods

Abstract

An antimicrobial composition of buckminsterfullerene with gallium phosphonate functional groups is provided to disassemble or make virus particles inert, and to inhibit viral and fungal proteases using catalytic desulfurization. This composition prevents and inactivates novel corona viruses including variant strains of SARS-Cov-2, fungal pathologies such as valley fever, respiratory ailments such as chronic obstructive pulmonary disorder (COPD), pneumonia, and arthropod vectored bacterial pathogens such as Lyme disease. The antiviral properties further prevent conditions leading to uncontrolled cellular proliferation, neoplasms, degenerative malignancy, cancers, and chronic inflammatory diseases. The gallium similarity to iron permits the treatment of osteoporosis, hypertension, and thrombosis by depolymerizing fibrin in the dissolution of clots and restoration of vascular plasticity. The composition can be produced at low temperatures through reactive shear milling. Delivery methods include ingestion, topical application, inhalation, or injection when used as a medicament or as a food supplement.

Description

CROSS-REFERENCE TO RELATED APPLICATION[0001]This application is a continuation of International Application PCT / US20 / 23024 filed on Mar. 16, 2020 which claims the benefit of U.S. provisional patent application 62 / 966,010 filed on Jan. 26, 2020, both of which are incorporated herein by reference in their entireties.BACKGROUND1. Field of Invention[0002]The present invention is a composition of buckminsterfullerene bonded with phosphonate pendant functional groups (FGP) being characterized by being size constrained and able to donate a gallium cation. The donated gallium ion serves to ion exchange with physiological sodium ions, thereby conferring a function as a nano-surfactant to the remaining fullerene phosphonate. The gallium ion synergistically confers an antimicrobial as well as an antioxidant property to the FGP. The composition of the invention can be used to prevent and treat thrombosis, to prevent or treat chronic respiratory illnesses such as pneumonia, and to help treat an ...

AI Technical Summary

Benefits of technology

[0017]This specification is directed in part to a composition comprising carbon fullerenes covalently derivatized with phosphonates having an oxidation state of three, where this substance is saponified with gallium atoms. The manufactured fullerene gallium phosphonates (FGP) provide antimicrobial, anti-cancer, anti-osteoporosis, and neurological therapeutics with additional viral and fungal protease inhibiting functions via the phosphonate sulfurization reaction. The donated gallium atoms are slowly displaced by ambient physiological sodium atoms. Both gallium and sodium confer nano-surfactant properties capable of reversibly shuttling between the oxygen groups of the phosphonate and the bare aromatic carbon face of the buckminsterfullerene by means of pi-cation bonding. These properties are useful to remediate thrombosis, blood clots, and treat hypertension. This composition also possesses the free radical scavenging chemical function of fullerenes, a viral capsid and spike protein disassembly function, and a biosurfactant function that couples with a pulmonary surfactant to reduce its viscosity and moderate cytokine and chemokine release. The composition can clear pulmonary surfactant and fibrins away from airway passages and remediate vascular fibrin mediated clotting reactions arising from the innate immune response to viruses such as novel corona viruses and the SARS-COV-2 virus variants. The result of the antimicrobial functions is to allow time for acquired immunity to be established as each new variant of rapidly evolving microbes is dissolved and disassembled for the body to learn a new immune response.

Problems solved by technology

Stroke, being one possible outcome of thrombosis, is the result of the intracerebral formation of fibrin clots and may lead to irreversible brain damage.

However, when such therapies are administered 4 to 6 hours after the onset of a stroke or heart attack, they fail to remove the blockages in time to rescue damaged tissues from a lack of oxygen and blood supply.

It is now well understood that viral spike glycoproteins, when presented by pathogenic invasions or by prophylactic mRNA induction, serve to worsen the systolic hypertension associated with hardening of the vasculature in aged persons, leading to a significant increase in mortality.

It is increasingly clear from epidemiology that the accrual of micro clots from multiple stressors including iron dysregulation may lead to stroke, neurological damage, kidney disease, and heart-attacks.

However, once divalent gallium or Ga2+ becomes trivalent gallium or Ga3+, it cannot biologically return to Ga2+, unlike iron, wherein the Fe2+ and Fe3+ are biologically reversible.

Except for an unusual organic complex of gallium that was reported to inhibit the SARS-COV-2 virus, there are no proactive strategies to eliminate either the symptoms or the associated pathologies for these virally induced conditions in medical or clinical practice.

Unfortunately, the use of gallium nitrate needs to be administered by continuous intravenous drip which is uncomfortable and inconvenient to patients.

Unfortunately, there are no known studies to possibly combine these two treatments.

However, aluminum nitrides of gallium have side effects that preclude these substances from being of long-term use to human patients, leaving the further development of a potential gallium mediated treatment for osteoporosis unexplored.

Gallium nitrate binds as transferrin-Ga3+ and stops DNA replication by depriving ribonucleotide reductase of iron by its presence, leading to cancer cell death while leaving healthy cells intact.

Further explorations of gallium found that the attraction was associative, especially when using an ultrasonic treatment, however these efforts failed in producing covalent bonds between C60 and gallium quantum dots.

Fullerene ruthenium phosphonates are reported to be useful for solar energy generation devices but are not known to be useful in a medical or a clinical use for patients or to treat any disease.

It is difficult to combat the virus inside one of these organisms when one of them is pathogenic and hidden within the other.

However, an intermediate combination of gallium and fullerene using phosphonates in a combined molecular structure has never been considered from a modelling perspective, or an experimental synthesis.

Therefore, nothing is currently known about such matters, except that sufficient scientific evidence establishes that any two of these substances can indeed react with each other.

Images